ATM/ATR

Signaling Pathway Map

Research Area

Inhibitory Selectivity
Solubility

Catalog No.	Product Name	Solubility(25°C)
Catalog No.	Product Name	Water	DMSO	Alcohol
S1009	Dactolisib (BEZ235, NVP-BEZ235)	<1 mg/mL	0.01 mg/mL	<1 mg/mL
S1092	KU-55933 (ATM Kinase Inhibitor)	<1 mg/mL	33 mg/mL	<1 mg/mL
S1570	KU-60019	<1 mg/mL	18 mg/mL	<1 mg/mL
S8007	VE-821	<1 mg/mL	74 mg/mL	<1 mg/mL
S2758	Wortmannin	<1 mg/mL	85 mg/mL	<1 mg/mL
S8729	AZ32	<1 mg/mL	66 mg/mL	7 mg/mL
S8680	AZD1390	<1 mg/mL	14 mg/mL	95 mg/mL
S8666	BAY 1895344 (BAY-1895344)	82 mg/mL	82 mg/mL	82 mg/mL
S2817	Torin 2	<1 mg/mL	20 mg/mL	<1 mg/mL
S2245	CP-466722	<1 mg/mL	0.28 mg/mL	<1 mg/mL
S7102	VE-822	<1 mg/mL	36 mg/mL	<1 mg/mL
S8050	ETP-46464	<1 mg/mL	6 mg/mL	<1 mg/mL
S7136	CGK 733	<1 mg/mL	100 mg/mL	<1 mg/mL
S7050	AZ20	<1 mg/mL	83 mg/mL	3 mg/mL
S7693	AZD6738	<1 mg/mL	82 mg/mL	41 mg/mL
S3600	Schisandrin B (Sch B)	<1 mg/mL	80 mg/mL	10 mg/mL
S8096	Mirin	<1 mg/mL	44 mg/mL	<1 mg/mL
S8375	AZD0156	<1 mg/mL	0.3 mg/mL	2 mg/mL
S4157	Chloroquine Phosphate	100 mg/mL	<1 mg/mL	<1 mg/mL

Isoform-specific Inhibitors

ATM/ATR Inhibitors (19)
New ATM/ATR Products

Catalog No.	Information	Product Use Citations	Product Validations
S1009	Dactolisib (BEZ235, NVP-BEZ235) Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3^TopBP1-ER cell.	Nature, 2018, 560(7718):372-376 Nature, 2017, 543(7647):728-732 Nature, 2017, 728-732	Level of phospho-proteins in RTK and PI3K–Akt–mTOR pathways in treated tumours, detected with western blot.
S1092	KU-55933 (ATM Kinase Inhibitor) KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor with IC50/K_i of 12.9 nM/2.2 nM in cell-free assays, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.	Nature, 2018, 560(7716):112-116 Nature, 2015, 528(7582):422-6 Nature, 2015, 10.1038/nature14328	Effects of NVP-BKM120 and KU-55933 and their combination on the DNA damage response. A, HCC1937 cells were treated for 18 hours with NVP-BKM120 at 2.5 μmol/L, KU-55933 at 10 μmol/L, or their combination, subjected to ionizing radiation(IR) with 10 Gy or mock, lysed 6 hours later, and subjected to immunoblotting with antibodies as indicated.
S1570	KU-60019 KU-60019 is an improved analogue of KU-55933, with IC50 of 6.3 nM for ATM in cell-free assays, 270- and 1600-fold more selective for ATM than DNA-PK and ATR,and is a highly effective radiosensitizer.	Nat Commun, 2016, 7:13701 Int J Cancer, 2015, 136(6):1445-57 Int J Cancer, 2013, 135(2):479-91	The ATM-dependent Ser15-p53 phosphorylation was monitored by Western blotting. Protein loading levels were monitored by probing for actin.
S8007	VE-821 VE-821 is a potent and selective ATP competitive inhibitor of ATR with K_i/IC50 of 13 nM/26 nM in cell-free assays, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ.	Nature, 2018, 555(7696):387-391 Nature, 2016, 539(7627):54-58 Nature, 2015, 518(7538):254-7	Cell viability response to ATR inhibitor.
S2758	Wortmannin Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays.	Nature, 2015, 10.1038/nature14412 Science, 2016, 353(6302):929-32 Cancer Res, 2014, 74(10):2846-56	L3.6pl cells at 6,000 cells per well were incubated in MEM with 5% FBS in triplicate in a 96-well culture plate and then treated alone with 5 umol/L BMS-777607, 10 umol/L wortmannin, or with BMS-777607 in combination with individual inhibitors. Polyploidy was examined under BK71 Olympus microscope and photographed 72 hours after treatment.
S8729^New	AZ32 AZ32 is a specific inhibitor of the ATM kinase that possesses good BBB penetration in mouse with an IC50 value of <0.0062 μM for ATM enzyme. It shows adequate selectivity over ATR and also has high cell permeability.
S8680^New	AZD1390 AZD1390 is a first-in-class orally available and CNS penetrant ATM inhibitor with an IC50 of 0.78 nM in cells and >10,000-fold selectivity over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases.
S8666^New	BAY 1895344 (BAY-1895344) BAY 1895344 is a potent, highly selective and orally available ATR inhibitor with an IC50 of 7 nM.
S2817	Torin 2 Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53−/− MEFs cell line; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively.	J Clin Invest, 2013, 124(2):742-54 Cell Rep, 2015, 11(3):446-59 Arterioscler Thromb Vasc Biol, 2018, 10.1161/ATVBAHA.118.311321	A. Western Blot analysis in the ALL-SIL cell line treated with single administration of Imatinib, Nilotinib, GZD824, Torin-2 and BGT226 for 24 h. An increase of expression of fast-migrating (lipidated) LC3A/B after drug treatments is shown. Twenty-five μg of protein were blotted on each lane. β-Actin documented equal lane loading. B. Flow cytometric analysis of autophagy in the ALL-SIL and PEER cell lines treated with single or combined administration of Imatinib, Nilotinib, GZD824 with Torin-2 or BGT226 for 24 h. CTRL, control (untreated) cells. Asterisks indicate significant differences in comparison to single drug treated samples (*p< 0.05). Imatinib, Nilotinib, GZD824, Torin-2 and BGT226 were abbreviated in IMA, NIL, GZD, TOR and BGT.
S2245	CP-466722 CP-466722 is a potent and reversible ATM inhibitor, does not affect ATR and inhibits PI3K or PIKK family members in cells.	PLoS One, 2015, 10(7):e0134411 PLoS One, 2012, 7(11):e50423 J Neurooncol, 2012, 110(3):349-57	HCT116 cells expressing the DDR-Act reporter were treated with Etoposide 20 μM (E20) for 24 hours, in the absence or in the presence of KU-55933 or CP-466722 at the indicated concentration. (A) Western blot analysis of p53 and actin as control.
S7102	VE-822 VE-822 is an ATR inhibitor with IC50 of 19 nM in HT29 cells.	J Virol, 2015, 10.1128/JVI.00389-15 Sci Rep, 2016, 6:27379	Flow cytometry analysis of E14.5 FL lineage negative cells from indicated genotypes treated with ATMi (KU-55933; 1nM), ATRi (VE-822; 1nM) or both inhibitors or DMSO as a negative control for 24 hours in culture before AnnexinV and PI levels were measured.
S8050	ETP-46464 ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.
S7136	CGK 733 CGK 733 is a potent and selective inhibitor of ATM/ATR with IC50 of ~200 nM.	Mol Cells, 2016, 39(12):869-876	K562 and K562R cells were pre-treated for 1 h with CGK733 (5 μM), then treated with CTD (10 μM) for 24 h, and protein levels of cleaved PARP, Mcl-1, and phosphorylated H3 were determined by Western blotting. GAPDH served as a normal control.
S7050	AZ20 AZ20 is a novel potent and selective inhibitor of ATR kinase with IC50 of 5 nM in a cell-free assay, 8-fold selectivity over mTOR.	Cell, 2018, 174(5):1127-1142 Mol Oncol, 2016, 10(5):751-63 Sci Rep, 2017, 7:41950	(B) SAHA treatment impairs the HR capacity of GBM03 cells. AZ20(ATRi) as a positive control.
S7693	AZD6738 AZD6738 is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.	J Dermatol Sci, 2016, 84(3):239-247 Sci Rep, 2017, 7:41950	AZD6738 (AZD) synergizes with cytarabine (ara-C) to induce apoptosis and proliferation inhibition in AML cells. (a) OCI-AML3 cells were treated with cytarabine and AZD6738, alone or in combination, for 24 h and then subjected to annexin V-FITC/PI staining and flow cytometry analyses. CI values were calculated using CompuSyn software. Combined drug treatments were compared to single drug treatment using 1-way ANOVA with Bonferroni post hoc test. ***indicates p < 0.001. (b and c) OCI-AML3 cells were treated with cytarabine and AZD-6738, alone or in combination, for 24 h. Whole cell lysates were subjected to Western blotting and probed with the indicated antibodies.
S3600	Schisandrin B (Sch B) Schisandrin B is the most abundant dibenzocyclooctadiene lignan present in the traditional Chinese medicinal herb Schisandra chinensis (Turcz.) Baill. It is a kind of ATR and P-gp inhibitor with high safety.
S8096	Mirin Mirin is a potent Mre11–Rad50–Nbs1 (MRN) complex inhibitor, and inhibits Mre11-associated exonuclease activity.
S8375	AZD0156 AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities.
S4157	Chloroquine Phosphate Chloroquine phosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator.	Leukemia, 2017, 10.1038/leu.2016.325 Cell Signal, 2016, 28(8):1086-98 Int J Mol Med, 2017, 10.3892/ijmm.2017.3008	NCI-H929 EV and miR-137 OE cells were treated with ATM activator Chloroquine Phosphate (CQ), specific ATM inhibitor KU-55933, and ATR inhibitor AZ20 for 12 hr. Immunoblotting showed the expression of p-ATM, p-Chk2, p-BRCA1, p-ATR and p-Chk1.

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ATM/ATR

Signaling Pathway Map

Research Area

Isoform-specific Inhibitors

Dactolisib (BEZ235, NVP-BEZ235)

KU-55933 (ATM Kinase Inhibitor)

KU-60019

VE-821

Wortmannin

AZ32

AZD1390

BAY 1895344 (BAY-1895344)

Torin 2

CP-466722

VE-822

ETP-46464

CGK 733

AZ20

AZD6738

Schisandrin B (Sch B)

Mirin

AZD0156

Chloroquine Phosphate